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ID: ALA1153454
Journal: Bioorg Med Chem
Title: Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs.
Authors: Moe ST, Thompson AB, Smith GM, Fredenburg RA, Stein RL, Jacobson AR.
Abstract: Botulinum neurotoxin elicits its paralytic activity through a zinc-dependant metalloprotease that cleaves proteins involved in neurotransmitter release. Currently, no drugs are available to reverse the effects of botulinum intoxication. Herein we report the design of a novel series of mercaptoacetamide small-molecule inhibitors active against botulinum neurotoxin serotype A. These analogs show low micromolar inhibitory activity against the isolated enzyme. Structure-activity relationship studies for a series of mercaptoacetamide analogs of 5-amino-3-phenylpyrazole reveal components essential for potent inhibitory activity.
CiteXplore: 19329331